Peptide Stapling through Site-Directed Conjugation of Triazine Moieties to the Tyrosine Residues of a Peptide
Y Zhang, R Yin, H Jiang, C Wang, X Wang… - Organic …, 2023 - ACS Publications
Organic Letters, 2023•ACS Publications
Peptide stapling is a strategy for improving the biological properties of peptides. Herein, we
report a novel method for stapling peptides that utilizes bifunctional triazine moieties for two-
component conjugation to the phenolic hydroxyl groups of tyrosine, which enables efficient
stapling of unprotected peptides. In addition, we applied this strategy to the RGD peptide
that can target integrins and demonstrated that the stapled RGD peptide had significantly
improved plasma stability and integrin-targeting ability.
report a novel method for stapling peptides that utilizes bifunctional triazine moieties for two-
component conjugation to the phenolic hydroxyl groups of tyrosine, which enables efficient
stapling of unprotected peptides. In addition, we applied this strategy to the RGD peptide
that can target integrins and demonstrated that the stapled RGD peptide had significantly
improved plasma stability and integrin-targeting ability.
Peptide stapling is a strategy for improving the biological properties of peptides. Herein, we report a novel method for stapling peptides that utilizes bifunctional triazine moieties for two-component conjugation to the phenolic hydroxyl groups of tyrosine, which enables efficient stapling of unprotected peptides. In addition, we applied this strategy to the RGD peptide that can target integrins and demonstrated that the stapled RGD peptide had significantly improved plasma stability and integrin-targeting ability.
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